Chemical structure

Related Biological Data

Related Biological Data

Biological Activity

Zebularine is a potent inhibitor of both DNA Methyltransferases and cytidine deaminase.

Targets

DNA Methyltransferases

cytidine deaminase

IC50

2 μM

Protocol

Cell experiment [1]:

Cell lines

10T1/2 cells

Preparation method

The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

30 μM; 24 hrs

Applications

In 10T1/2 cells, Zebularine induced muscle cell formation. However, the 10T1/2 cells treated with Zebularine showed less muscle cell formation than those treated with either 5-Aza-CdR or 5-Aza-CR.

Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request

General tips

For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Zebularine, a chemically stable cytidine analog containing a 2-(1H)-pyridimidinone ring, is an effective DNA methylation inhibitor which can act with DNA methyltransferases to form a covalent complex. It has been shown to cause demethylation and reactivation of a silenced and hypermethylated p16 gene. Zebularine is able to induce the myogenic phenotype in 10T1/2 cells, which is a phenomenon unique to DNA methylation inhibitors. zebularine can act as a pro-drug leading to inhibition of DNA methylation and gene activation in fungal and mammalian cells. It was the only slightly cytotoxic to T24 cells in vitro. Zebularine is stable in aqueous solution up to a pH of 12.